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Asthma control
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Therapeutic index
Efficacy is paramount to offering a suitable asthma treatment for your patients – but it shouldn’t come at the expense of safety. Therapeutic index is a measure of benefit vs risk which, in the case of asthma medications, can be defined as the ratio of systemic activity (cortisol suppression) / airway potency (efficacy).1 It may be a useful measure to demonstrate therapeutic differences between medications and help guide treatment decisions.1
Relvar has a wide therapeutic index thanks to its unique molecular profile, most notably its high receptor binding affinity.1 The result is an asthma treatment that treats underlying inflammation*†1 and provides long-lasting bronchodilation,*2 with very little systemic effect.*†1
Receptor binding affinity
The receptor binding affinity of a treatment is an important characteristic in its ability to provide a medicinal benefit, particularly when it comes to the anti-inflammatory effect of an ICS.3
In vitro data show that fluticasone furoate has a higher glucocorticoid receptor binding affinity vs other commonly prescribed ICS’s.*3
Relationship between glucocorticoid receptor binding affinity and the therapeutic index for various ICS dose regimens*3
LOCs to purchase copyrights for the reuse of this graph within their markets. Please ensure the correct statement is included to comply with the terms of the licence. It was first published in Daley-Yates PT. Br J Clin Pharmacol 2015;80:372–380. British Journal of Clinical Pharmacology published by John Wiley & Sons Ltd on behalf of The British Pharmacological Society.
Bronchodilation remains persistent with vilanterol2
Airway protection and systemic effects
A treatment's receptor binding affinity is not the only factor that can influence its therapeutic index – systemic effects are also an important factor.1
Relvar’s ICS treats underlying inflammation, with more airway protection and less systemic effect vs budesonide.*1
20% cortisol suppression is the lowest boundary of detectable systemic exposure for corticosteroids, after which systemic adverse events become more likely.3
Therapeutic index of inhaled corticosteroids in asthma: A dose–response comparison on airway hyperresponsiveness and adrenal axis suppression, Daley-Yates P, et al. Copyright © 2020 The Authors. Reproduced with permission of John Wiley & Sons Ltd.
This was an escalating dose, placebo-controlled, incomplete block, two-period, crossover study of patients aged 18–65 with a history of bronchial asthma first diagnosed at least 6 months prior to screening (N=54). The primary objective of the study was to characterise the dose-response and relative potency of FF, FP and BUD in reducing airway hyperresponsiveness via AMP challenge (AMP PC20). The therapeutic index was calculated by dividing the ED50 cortisol suppression by the ED50 AMP PC20.1
Fluticasone furoate and vilanterol are not licensed as monotherapies for patients with asthma in all markets.
Relative airway potency of FF was higher than predicted from its relative glucocorticoid receptor (GR) binding affinity vs FP and BUD.1 This may be due to:
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Footnotes
*In vitro data: clinical relevance is uncertain.
†Note that this study also included unlicensed doses of budesonide and fluticasone propionate – see full reference for details.1
‡BUD 200 μg BD, 23.91 (95% CI 15.08–37.90) vs FF 100 μg OD, 81.45 (95% CI 44.65–148.58).
Abbreviations
AE, adverse event; AMP PC20, provocative concentration of adenosine 5'-monophosphate that induces a 20% decline in forced expiratory volume in one second; BD, twice daily; BUD, budesonide; CI, confidence interval; ED50, median effective dose; FF, fluticasone furoate; FP, fluticasone propionate; GR, glucocorticoid receptor; ICS, inhaled corticosteroid; OD, once daily; TI, therapeutic index.
Relvar Safety Information4
Contraindications
Hypersensitivity to the active substances or to any of the excipients.
Undesirable effects
Very Common: Headache, Nasopharyngitis.
Common: Infections and infestations, Oropharyngeal pain, Sinusitis, Pharyngitis, Rhinitis, Cough, Dysphonia, Abdominal pain, Arthralgia, Back pain, Fractures, Muscle spasms and Pyrexia.
References
- Daley-Yates P, et al. Br J Clin Pharmacol 2021;87:483–493.
- Slack RJ, et al. Pharmacol Exp Ther 2013;344:218–230.
- Daley-Yates P. Br J Clin Pharmacol 2015;80:372–380.
- Relvar Prescribing Information.
GSK does not recommend, endorse, or accept liability for the 3rd party sites.
For more information, please refer to the prescribing information or contact GlaxoSmithKline via gcc.medinfo@gsk.com
To report Adverse Event/s associated with the use of GSK product/s, please contact us via
gulf.safety@gsk.com
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Gulf.ProductQualityComplaints@gsk.com
Department of Pharmacovigilance & Drug Information |
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PM-RCH-FFV-WCNT-250001 Date of preparation: July 2025
